Nuclear-receptor ligands and ligand-binding domains

被引:271
作者
Weatherman, RV [1 ]
Fletterick, RJ
Scanlan, TS
机构
[1] Univ Calif San Francisco, Dept Pharmaceut Chem, San Francisco, CA 94143 USA
[2] Univ Calif San Francisco, Dept Biochem & Biophys, San Francisco, CA 94143 USA
[3] Univ Calif San Francisco, Dept Mol & Cellular Pharmacol, San Francisco, CA 94143 USA
关键词
intracellular receptors; steroid/thyroid hormone receptors; transcriptional regulation; intracellular signaling; hormone agonists/antagonists;
D O I
10.1146/annurev.biochem.68.1.559
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
The determination of several structures of nuclear receptor ligand binding domains (LBD) has led to new insights into the mechanism of action of this very important class of receptors. This review describes and compares the different LED structures and their relationship to the function of the nuclear receptors. The role of the ligand in the LED structures and the implications of ligand structure on receptor activity are also discussed. Structural information regarding interactions between the LED and coactivator proteins and the potential role of these interactions in ligand agonism and antagonism is reviewed. Different pathways for nuclear receptor signaling and the use of new ligands to investigate these pathways are also described.
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页码:559 / 581
页数:23
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